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valemetostat 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| histone N-methyltransferase inhibitors | 5724 | 1809336-39-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Valemetostat is a drug that blocks two enzymes called EZH1 and EZH2. These enzymes are involved in the growth of some blood cancers and solid tumors, such as non-Hodgkin lymphomas (NHL). Valemetostat is used to treat a type of NHL called adult T-cell leukaemia/lymphoma (ATL) that has come back or does not respond to other treatments.
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.737 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 39.719 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.798 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 2.673 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 30.100 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 36.950 | % | High | 1 |
| herg | hERG pIC50 | 4.429 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.125 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 20.370 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 26.680 | % | High | 1 |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 9.727 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 23.714 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 23.690 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 16.749 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 42.400 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 12.417 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 56.070 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 32.720 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 862.979 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 26, 2022 | PMDA | DAIICHI SANKYO COMPANY, LIMITED |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Relapsed or refractory T-cell leukemia-lymphoma | indication | 110007008 | DOID:5603 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Histone-lysine N-methyltransferase EZH2 | Enzyme | INHIBITOR | IC50 | 8.22 | SCIENTIFIC LITERATURE | ||||
| Histone-lysine N-methyltransferase EZH1 | Enzyme | INHIBITOR | IC50 | 8 | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| CHEBI:758103 | CHEBI |
| CHEMBL4597193 | ChEMBL_ID |
| 12282 | IUPHAR_LIGAND_ID |
| C5239419 | UMLSCUI |
| CHEMBL4594405 | ChEMBL_ID |
| 10747 | INN_ID |
| 126481870 | PUBCHEM_CID |
| D11551 | KEGG_DRUG |
| 60RD0234VE | UNII |
Pharmaceutical products:
None